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奥替拉西林-载 Soluplus-Pluronic P105 混合胶束口服制剂的优化与评价。

Optimization and evaluation of Oridonin-loaded Soluplus-Pluronic P105 mixed micelles for oral administration.

机构信息

Nanjing University of Chinese Medicine, Nanjing, Jiangsu, 210023, China; College of Chemistry and Chemical Engineering, Huangshan University, Huangshan, Anhui, 245041, China; Key Laboratory of New Drug Delivery System of Chinese Material Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, 210028, China.

Key Laboratory of New Drug Delivery System of Chinese Material Medica, Jiangsu Provincial Academy of Chinese Medicine, Nanjing, Jiangsu, 210028, China.

出版信息

Int J Pharm. 2017 Feb 25;518(1-2):193-202. doi: 10.1016/j.ijpharm.2016.12.047. Epub 2016 Dec 22.

Abstract

In this study, a new type of mixed micelles was developed using Soluplus (SOL) and Pluronic P105 (P105) for the encapsulation of Oridonin (ORN). Oridonin-loaded micelles (ORN-M) were simply prepared using solvent evaporation and characterized for particle size, particle morphology, encapsulation efficiency, and drug loading. In addition, the in vitro drug release behavior of ORN-M was assessed using the widely applied dialysis bag technique. The pharmacokinetic property of ORN was explored in rats after oral administration of ORN-M. Optimized ORN-M were of a small size (137.2±1.65nm) and spherical shape when the ratio of SOL:P105 was 3:1, with entrapment efficiency 90.48±1.85% and drug loading 15.08±0.38%. Oral absorption capacity of ORN was greatly enhanced with a relative bioavailability of 210.55% in comparison to that of in-house suspensions, which suggests that ORN-M shows significantly improved bioavailability and drug absorption characteristics. Overall, the optimized SOL-P105 dual mixed micelles show great potential for use as oral drug carriers for cancer treatment.

摘要

在这项研究中,使用 Soluplus(SOL)和 Pluronic P105(P105)开发了一种新型混合胶束,用于包封冬凌草甲素(ORN)。采用溶剂蒸发法制备冬凌草甲素载药胶束(ORN-M),并对其粒径、颗粒形态、包封率和载药量进行了表征。此外,还采用广泛应用的透析袋技术评估了 ORN-M 的体外药物释放行为。通过大鼠口服 ORN-M 研究了 ORN 的药代动力学性质。当 SOL:P105 的比例为 3:1 时,优化的 ORN-M 的粒径为 137.2±1.65nm,呈球形,包封效率为 90.48±1.85%,载药量为 15.08±0.38%。与内部混悬剂相比,冬凌草甲素的口服吸收能力大大增强,相对生物利用度为 210.55%,这表明 ORN-M 具有显著提高的生物利用度和药物吸收特性。总的来说,优化的 SOL-P105 双混合胶束具有作为癌症治疗口服药物载体的巨大潜力。

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